专利号:EP-0439404-B1 优先权日:1990-01-25 标题 :Preparation of 2-(2'-thienyl) alkylamines and derivatives thereof and synthesis of 4,5,6,7- thieno [3,2-c] pyridine derivatives therefrom 发明人:KHATRI HIRALAL N; DEHOFF BRADLEY S 权利人:SANOFI SA 摘要:An improved process for the synthesis of 2-(2 min -thienyl)ethylamine from suitably functionalized derivatives of 2-(2 min -thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2 min -thienyl)ethylamine produced by this process is advantageously converted to the carbamic acid salt, which is suitably reconverted to 2-(2 min -thienyl)ethylamine, a useful intermediate in the synthesis of ticlopidine.
专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:US-5068360-A 优先权日:1990-01-25 标题 :Preparation of 2-(2'-thienyl)ethylamine derivatives and synthesis of thieno(3,2-C)pyridine derivatives therefrom 发明人:DEHOFF BRADLEY S 权利人:SYNTEX INC 摘要:An improved process for the synthesis of 2-(2'-thienyl)ethylamine from suitably functionalized derivatives of 2-(2'-thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2'-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.
专利号:US-5191090-A 优先权日:1990-01-25 标题:Preparation of 2-(2'-thienyl)ethylamine derivatives and synthesis of thieno[3,2-c]pyridine derivatives therefrom 发明人:DEHOFF BRADLEY S 权利人:SYNTEX INC 摘要:An improved process for the synthesis of 2-(2'-thienyl)ethylamine from suitably functionalized derivatives of 2-(2'-thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2'-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.
专利号:US-7342003-B2 优先权日:2001-10-25 标 题 :Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs 发明人:MOORMAN ALLAN R; SCANNELL MICHAEL; BALASUBRAMANIAN THIAGARAJAN; OUTCALT RUSSELL; LEUNG EDWARD 权利人:KING PHARMACEUTICALS RES & DEV 摘要:Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.
专利号:US-9765027-B2 优先权日:2014-08-22 标题 :Substituted 1-arylethyl-4-acylaminopiperidine derivatives as opioid/alpha-adrenoreceptor modulators and method of their preparation 发明人:VARDANYAN RUBEN S; HRUBY VICTOR J 权利人:THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZAONA; UNIV ARIZONA 摘要:The invention provides compounds that bind with high affinities to the μ-, δ- and κ-opioid receptors and α 2 -adrenoreceptor. In addition to providing these compounds with novel pharmacological binding properties, the invention also describes detailed novel methods for the preparation of representative compounds and a scheme for the synthesis of related compounds that bind to the opioid receptors and/or α 2 -adrenoreceptor.
[参考文献]: Radoslaw Laufer, Et Al. Discovery Of Inhibitors Of The Mitotic Kinase Ttk Based On N-(3-(3-Sulfamoylphenyl)-1H-Indazol-5-Yl)-Acetamides And Carboxamides. Bioorg Med Chem. 2014 Sep 1;22(17):4968-97.
合成参考文献
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